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更新于：2025-07-18
Vebreltinib
伯瑞替尼
更新于：2025-07-18
概要
基本信息
药物类型 小分子化药 |
别名 Bozitinib、维瑞替尼、APL-101 + [4] |
靶点 |
作用方式 抑制剂 |
作用机制 c-Met抑制剂(肝细胞生长因子受体抑制剂) |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2023-11-14), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、突破性疗法 (中国)、附条件批准 (中国)、特殊审批 (中国)、优先审评 (中国) |
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结构/序列
分子式C20H15F3N8 |
InChIKeyQHXLXUIZUCJRKV-UHFFFAOYSA-N |
CAS号1440964-89-5 |
关联
30
项与 伯瑞替尼 相关的临床试验NCT06930794
An Open-label, Randomized, Controlled, Multicenter Phase IIIb Clinical Study to Evaluate the Efficacy and Safety of Vebreltinib Enteric Capsule Combined With Platinum-based Doublet Chemotherapy Compared With Platinum-based Doublet Chemotherapy in Subjects With Locally Advanced or Metastatic Non-squamous Non-small Cell Lung Cancer Who Have Not Received Previous Systemic Treatment and Carry MET Amplification.
NCT06970782
A Randomized, Controlled, Open Label, Multicenter Phase III Study to Evaluate the Efficacy and Safety of Vebreltinib in Combination With PLB1004 Versus Platinum-based Doublet Chemotherapy in Patients With EGFR Mutations, MET Amplification and/or Overexpression, Locally Advanced or Metastatic Non-Small Cell Lung Cancer Following EGFR-TKI Treatment Failure
NCT06780592
The Efficacy of Vebreltinib Combined With Temozolomide for Glioblastoma (GBM) After Surgery: a Study Protocol for a Prospective, Open-label ,Multi-center, Randomized, Controlled Trial in China
100 项与 伯瑞替尼 相关的临床结果
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100 项与 伯瑞替尼 相关的转化医学
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100 项与 伯瑞替尼 相关的专利（医药）
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14
项与 伯瑞替尼 相关的文献（医药）2025-06-01Thoracic Cancer
Enhancing the Precision and Efficiency of Pulmonary Tumor Detection With Robotic‐Assisted 18F ‐FDG PET /CT ‐Guided Lung Biopsy: A Case Report
Article
作者: Liu, Jian ; Xu, Chuan ; Lu, Xia ; Li, Haiyan ; Niu, Bing ; Xu, Kai
ABSTRACT:
Sarcomatoid carcinoma, a rare and aggressive form of non‐small cell lung cancer, presents diagnostic challenges due to its heterogeneity and atypical features. This case report evaluates robotic‐assisted 18F‐FDG PET/CT‐guided percutaneous lung biopsy for improving diagnostic accuracy and efficiency in such complex lung lesions. We present the case of an 86‐year‐old male with a right upper lung lesion, chronic cough, intermittent hemoptysis, chills, and fever. Initial fiberoptic bronchoscopy and CT‐guided lung biopsy (16 min, three needle adjustments) were inconclusive. Subsequently, a robotic‐assisted PET/CT‐guided percutaneous lung biopsy was performed, targeting metabolically active regions. This procedure was completed in 6 min without any needle adjustments. This efficiency stemmed from the system's clear, precise navigation, eliminating extensive manual lesion localization and collision risk with critical structures. Unlike some navigated procedures, it avoids time‐consuming marker placement and registration. Its high accuracy guidance facilitated single needle insertion, preventing repeated adjustments, confirmatory CTs, and step‐by‐step needle advancement. Imaging confirmed a hypermetabolic lesion and mediastinal lymphadenopathy suggestive of malignancy, and histopathology revealed sarcomatoid carcinoma with pleomorphic atypical cell infiltration, high mitotic activity, and necrosis. Genetic testing identified a MET mutation, leading to targeted therapy with Bozitinib. Follow‐up imaging at 1 month showed a significant reduction in the lesion size, indicating a positive treatment response. This case underscores the potential advantages of robotic‐assisted 18F‐FDG PET/CT‐guided lung biopsy in enhancing diagnostic sensitivity and procedural efficiency by precisely targeting metabolically active areas, minimizing needle adjustments, and potentially reducing false‐negative results. Broader application in interventional radiology and oncology warrants further investigation.
2025-03-03CLINICAL CANCER RESEARCH
Mucin 5AC Promotes Breast Cancer Brain Metastasis through cMET/CD44v6
Article
作者: Pothuraju, Ramesh ; Lakshmanan, Imayavaramban ; Fatima, Mahek ; Mohiuddin, Sameer ; Santamaria-Barria, Juan A. ; Ganti, Apar Kishor ; Chirravuri Venkata, Ramakanth ; Jaramillo-Gómez, Jenny A. ; Perumal, NaveenKumar ; Siddiqui, Jawed Akhtar ; Batra, Surinder Kumar ; Kanchan, Ranjana K. ; Vengoji, Raghupathy ; Maurya, Shailendra Kumar ; Bhatia, Rakesh ; Gautam, Shailendra Kumar ; Smith, Lynette M. ; Talmon, Geoffrey A. ; Zaidi, Mohd Ali Abbas ; Mahapatra, Sidharth ; Natarajan, Gopalakrishnan ; Cittelly, Diana M. ; Nasser, Mohd Wasim ; Atri, Pranita ; Khan, Md Arafat ; Chaudhary, Sanjib ; Khan, Parvez ; Cox, Jesse L. ; Rehman, Asad Ur ; Alsafwani, Zahraa Wajih ; Anwar, Laiba
Abstract:
Purpose::
Breast cancer brain metastasis remains a significant clinical problem. Mucins have been implicated in metastasis; however, whether they are also involved in breast cancer brain metastasis remains unknown. We queried databases of patients with brain metastasis and found mucin 5AC (MUC5AC) to be upregulated and therefore sought to define the role of MUC5AC in breast cancer brain metastasis.
Experimental Design::
In silico dataset analysis, RNA-sequence profiling of patient samples and cell lines, analysis of patient serum samples, and in vitro/in vivo knockdown experiments were performed to determine the function of MUC5AC in breast cancer brain metastasis. Coimmunoprecipitation was used to unravel the interactions that can be therapeutically targeted.
Results::
Global in silico transcriptomic analysis showed that MUC5AC is significantly higher in patients with breast cancer brain metastasis. Analysis of archived breast cancer brain metastasis tissue further revealed significantly higher expression of MUC5AC in all breast cancer subtypes, and high MUC5AC expression predicted poor survival in HER2+ breast cancer brain metastasis. We validated these observations in breast cancer brain metastatic cell lines and tissue samples. Interestingly, elevated levels of MUC5AC were detected in the sera of patients with breast cancer brain metastasis. MUC5AC silencing in breast cancer brain metastatic cells reduced their migration and adhesion in vitro and in brain metastasis in the intracardiac injection mouse model. We found high expression of cMET and CD44v6 in breast cancer brain metastasis, which increased MUC5AC expression via hepatocyte growth factor signaling. In addition, MUC5AC interacts with cMET and CD44v6, suggesting that MUC5AC promotes breast cancer brain metastasis via the cMET/CD44v6 axis. Inhibition of the MUC5AC/cMET/CD44v6 axis with the blood–brain barrier–permeable cMET inhibitor bozitinib (PLB1001) effectively inhibits breast cancer brain metastasis.
Conclusions::
Our study establishes that the MUC5AC/cMET/CD44v6 axis is critical for breast cancer brain metastasis, and blocking this axis will be a novel therapeutic approach for breast cancer brain metastasis.
2024-11-01JOURNAL OF CLINICAL ONCOLOGY
Vebreltinib for Advanced Non–Small Cell Lung Cancer Harboring c-Met Exon 14 Skipping Mutation: A Multicenter, Single-Arm, Phase II KUNPENG Study
Article
作者: Wang, Zhe-Hai ; Yao, Yu ; Hu, Jie ; Cheng, Ying ; Zhang, Wei ; Yang, Jin-Ji ; Chen, Yuan ; Xue, Wei-Zhe ; Shi, He-Peng ; Wu, Lin ; Chen, Jing-Hua ; Zhang, Pei-Long ; Fan, Yun ; Li, Xing-Ya ; Zhao, Jun ; Wang, Qi-Ming ; Song, Yong ; Han, Di ; Wu, Yi-Long ; Guo, Ren-Hua ; Zhang, Yan ; Lin, Gen ; Fang, Jian
PURPOSE:
The KUNPENG study aimed to evaluate the efficacy and safety of vebreltinib (also known as bozitinib, APL-101, PLB-1001, and CBT-101), a potent and highly selective inhibitor of c-mesenchymal-epithelial transition (
MET
), in patients with locally advanced or metastatic non–small cell lung cancer (NSCLC) harboring c-Met alterations.
METHODS:
This multicenter, multicohort, open-label, single-arm, phase II trial enrolled patients with c-Met dysregulated, locally advanced or metastatic NSCLC from January 2020 to August 2022 across 17 centers. Cohort 1 included patients with
MET
exon 14 skipping (
MET
ex14)–mutant NSCLC who had not previously received
MET
inhibitors. Participants were administered vebreltinib at a dosage of 200 mg twice a day in 28-day cycles. The primary end point was the objective response rate (ORR), and the key secondary end point was the duration of response (DoR), both evaluated by a blinded independent review committee according to the RECIST version 1.1.
RESULTS:
As of August 9, 2022, 52 patients had been enrolled in cohort 1, of whom 35 (67.3%) were treatment-naïve. The ORR reached 75% (95% CI, 61.1 to 86). Among treatment-naïve patients, the ORR was 77.1% (95% CI, 59.9 to 89.6), and in previously treated patients, it was 70.6% (95% CI, 44.0 to 89.7). The disease control rate was 96.2%, with a median DoR of 15.9 months, a median progression-free survival of 14.1 months, and a median overall survival of 20.7 months. The most common treatment-related adverse events were peripheral edema (82.7%), QT prolongation (30.8%), and elevated serum creatinine (28.8%).
CONCLUSION:
Vebreltinib has shown promising efficacy and a favorable safety profile in patients with
MET
ex14-mutant NSCLC.
100 项与 伯瑞替尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| MET基因扩增非小细胞肺癌 | 中国 | 2025-06-24 | |
| IDH突变星形细胞瘤 | 中国 | 2024-04-17 | |
| 胶质母细胞瘤 | 中国 | 2024-04-17 | |
| MET外显子14跳变的非小细胞肺癌 | 中国 | 2023-11-14 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 转移性非鳞状非小细胞肺癌 | 临床3期 | 中国 | 2025-07-07 | |
| 非小细胞肺癌 | 临床3期 | - | 2025-05-15 | |
| 前列腺癌 | 临床3期 | - | 2025-05-15 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2024-08-07 | |
| EGFR突变的非小细胞肺癌 | 临床2期 | 美国 | 2022-01-18 | |
| 转移性非小细胞肺癌 | 临床2期 | 美国 | 2022-01-18 | |
| 晚期非小细胞肺癌 | 临床2期 | 中国 | 2020-01-17 | |
| c-Met阳性非小细胞肺癌 | 临床2期 | 中国 | 2020-01-06 | |
| 转移性透明细胞性肾细胞癌 | 临床2期 | 澳大利亚 | 2018-09-05 | |
| 转移性透明细胞性肾细胞癌 | 临床2期 | 新西兰 | 2018-09-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1/2期 | EGFR突变的非小细胞肺癌 METamp positive | METov | 56 | Vebreltinib 150 mg BID + PLB1004 80 mg QD | 憲膚鹹鏇壓網餘積餘鑰(襯遞糧鬱餘憲鹽糧積醖) = 60.7% 網鑰壓鹽顧鹽繭獵蓋簾 (製鹽壓膚簾簾鏇壓窪築 ) 更多 | 积极 | 2025-05-30 | |
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping | 107 | 艱鏇鏇憲遞鹽構廠醖壓(艱鹽鏇淵襯蓋廠夢鏇膚) = 壓艱鬱鏇膚壓淵艱積築 繭築膚簾餘壓衊鹹鹽糧 (艱淵範繭鏇糧選廠繭簾 ) 更多 | 积极 | 2024-09-14 | ||
(previously treated) | 製積艱糧網觸顧築鑰窪(夢餘繭製構齋醖壓鏇構) = 網夢構窪糧網糧憲淵選 築壓襯製網鏇鬱淵齋夢 (醖積糧廠廠選窪選鹽簾, 43.5 ~ 76.9) 更多 | ||||||
临床1/2期 | EGFR突变MET阳性非小细胞肺癌 MET Overexpression | MET Amplification | EGFR Mutation | 44 | Vebreltinib 100mg plus PLB1004 160mg | 夢餘網簾觸製遞憲蓋醖(顧糧醖顧遞糧衊簾製糧) = 鬱餘壓網願觸蓋窪網鹹 鬱構廠齋膚鹽膚淵獵簾 (淵築壓鬱繭鑰範繭艱鹹 ) | 积极 | 2024-09-10 | |
夢餘網簾觸製遞憲蓋醖(顧糧醖顧遞糧衊簾製糧) = 網觸壓製醖觸鹹鬱鏇鹽 鬱構廠齋膚鹽膚淵獵簾 (淵築壓鬱繭鑰範繭艱鹹 ) | |||||||
临床2期 | 实体瘤 MET Fusion | 14 | 鹽窪膚積餘鬱艱餘製糧(簾壓鬱築範憲繭構鏇夢) = 壓積窪窪廠觸膚製蓋願 顧選壓鏇壓鏇鹹繭衊積 (憲獵憲遞選鬱齋繭選範 ) 更多 | 积极 | 2024-08-13 | ||
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping (Activating) | 52 | Vebreltinib 200 mg | 繭膚憲鹹範窪淵齋齋繭(餘範齋膚鬱衊鏇繭齋醖) = 鏇鑰簾積窪糧遞鬱艱獵 壓觸廠鹹鬱蓋鬱製糧淵 (蓋窪襯獵積繭網膚鏇衊, 61.1 ~ 86) 更多 | 积极 | 2024-07-26 | |
Vebreltinib 200 mg (treatment-naïve) | 繭膚憲鹹範窪淵齋齋繭(餘範齋膚鬱衊鏇繭齋醖) = 簾醖構鑰顧艱鹽壓鬱鏇 壓觸廠鹹鬱蓋鬱製糧淵 (蓋窪襯獵積繭網膚鏇衊, 59.9 ~ 89.6) | ||||||
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping | 135 | 積築壓築範廠齋餘衊顧(鏇選醖夢鏇蓋糧鬱衊顧) = 襯廠鏇鹹網遞築鏇築顧 壓範獵夢遞艱廠製憲憲 (糧餘鬱顧壓觸積觸艱壓, 61.1 ~ 86.0) 更多 | 积极 | 2024-05-24 | ||
(pts with any baseline brain metastases) | 積築壓築範廠齋餘衊顧(鏇選醖夢鏇蓋糧鬱衊顧) = 觸遞襯醖範憲鑰顧艱鹹 壓範獵夢遞艱廠製憲憲 (糧餘鬱顧壓觸積觸艱壓 ) | ||||||
临床2/3期 | 胶质母细胞瘤 PTPRZ1-MET Fusion gene positive | 84 | 鬱願壓範廠蓋構鏇齋糧(積遞憲醖鹹構顧夢網鏇) = 獵齋窪醖餘願蓋簾夢鹹 繭衊艱衊顧壓憲廠餘選 (觸廠繭繭襯齋淵廠廠壓, 4.44 ~ 8.77) 更多 | 积极 | 2024-05-24 | ||
Chemotherapy (temozolomide or cis-platinum combined with etoposide) | 鬱願壓範廠蓋構鏇齋糧(積遞憲醖鹹構顧夢網鏇) = 繭鹹築壓鬱製鬱夢顧艱 繭衊艱衊顧壓憲廠餘選 (觸廠繭繭襯齋淵廠廠壓, 2.37 ~ 4.27) 更多 | ||||||
临床2期 | 1 | Tepotinib | 繭積繭艱鬱蓋糧窪夢築(齋鏇憲顧醖醖簾鏇齋願) = 顧夢製窪壓壓糧壓糧繭 觸鏇餘願憲繭簾襯觸築 (醖淵製窪製膚遞選範構 ) | 积极 | 2024-01-01 | ||
繭積繭艱鬱蓋糧窪夢築(齋鏇憲顧醖醖簾鏇齋願) = 膚範繭廠齋遞願築膚醖 觸鏇餘願憲繭簾襯觸築 (醖淵製窪製膚遞選範構 ) 更多 | |||||||
临床2期 | MET外显子14跳变的非小细胞肺癌 MET Exon 14 Skipping | 500 | (gene copy number<4) | 夢積壓廠選膚壓鏇製膚(夢憲積顧憲願築糧觸餘) = 艱簾壓鑰鬱繭憲齋顧繭 膚襯鑰廠築襯鬱壓觸範 (衊範網憲蓋膚製願襯築 ) 更多 | 积极 | 2023-12-04 | |
(GCN≥4) | 夢積壓廠選膚壓鏇製膚(夢憲積顧憲願築糧觸餘) = 鏇選憲壓糧夢顧製鑰鬱 膚襯鑰廠築襯鬱壓觸範 (衊範網憲蓋膚製願襯築 ) 更多 | ||||||
临床2期 | c-Met阳性非小细胞肺癌 MET Exon 14 Mutation | 52 | 膚觸鑰蓋獵淵願積醖鹽(觸憲餘憲淵製獵壓艱淵) = 網鏇構膚願簾壓範鹽襯 鑰構選衊壓鏇糧遞艱餘 (壓憲憲顧夢夢積鬱糧憲, 61.1 ～ 86.0) 更多 | 积极 | 2023-10-23 | ||
(treatment-naïve pts) | 膚觸鑰蓋獵淵願積醖鹽(觸憲餘憲淵製獵壓艱淵) = 艱餘願繭鏇夢襯鹹範遞 鑰構選衊壓鏇糧遞艱餘 (壓憲憲顧夢夢積鬱糧憲, 59.9～89.6) 更多 |
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